Metabolism of tamoxifen by recombinant human cytochrome P450 enzymes: formation of the 4-hydroxy, 4′-hydroxy andN-desmethyl metabolites and isomerization …
HK Crewe, LM Notley, RM Wunsch, MS Lennard… - Drug metabolism and …, 2002 - ASPET
The cytochrome P450 (P450)-mediated biotransformation of tamoxifen is important in
determining both the clearance of the drug and its conversion to the active metabolite,trans-4-…
determining both the clearance of the drug and its conversion to the active metabolite,trans-4-…
Oxidation phenotype—a major determinant of metoprolol metabolism and response
MS Lennard, JH Silas, S Freestone… - … England Journal of …, 1982 - Mass Medical Soc
GENETIC polymorphism in the oxidative metabolism of debrisoquine 1 is largely responsible
for individual differences in its plasma concentration and antihypertensive effect. Poor …
for individual differences in its plasma concentration and antihypertensive effect. Poor …
Influence of dose, cigarette smoking, age, sex, and metabolic activity on plasma clozapine concentrations: a predictive model and nomograms to aid clozapine dose …
…, AM Amin, EP Spencer, MS Lennard… - Journal of clinical …, 2004 - journals.lww.com
… Sachse C, Brockmoller J, Bauer S, et al. Functional significance of a CA polymorphism in
intron 1 of the cytochrome P450 CYP1A2 gene tested with caffeine. Br J Clin Pharmacol …
intron 1 of the cytochrome P450 CYP1A2 gene tested with caffeine. Br J Clin Pharmacol …
Variable contribution of cytochromes P450 2D6, 2C9 and 3A4 to the 4-hydroxylation of tamoxifen by human liver microsomes
HK Crewe, SW Ellis, MS Lennard, GT Tucker - Biochemical pharmacology, 1997 - Elsevier
4-Hydroxylation is an important pathway of tamoxifen metabolism because the product of this
reaction is intrinsically 100 times more potent as an oestrogen receptor antagonist than is …
reaction is intrinsically 100 times more potent as an oestrogen receptor antagonist than is …
The generation, detection, and effects of reactive drug metabolites
…, J Farrell, DJ Naisbitt, MS Lennard - Medicinal research …, 2013 - Wiley Online Library
The decline in approval of new drugs during the past decade has led to a close analysis of
the drug discovery process. One of the main reasons for attrition is preclinical toxicity, …
the drug discovery process. One of the main reasons for attrition is preclinical toxicity, …
[HTML][HTML] Evidence that aspartic acid 301 is a critical substrate-contact residue in the active site of cytochrome P450 2D6
…, MJ Ackland, MJE Sternberg, MS Lennard… - Journal of Biological …, 1995 - ASBMB
Model building studies have intimated a role for aspartic acid 301 in the substrate binding of
cytochrome P450 2D6 (CYP2D6). We have tested this hypothesis by generating a range of …
cytochrome P450 2D6 (CYP2D6). We have tested this hypothesis by generating a range of …
[HTML][HTML] Monitoring plasma concentrations to individualize treatment with clomiphene citrate
A Rostami-Hodjegan, MS Lennard, GT Tucker… - Fertility and sterility, 2004 - Elsevier
OBJECTIVE: Recent reports have indicated that a number of individual patient characteristics
are responsible for the success or failure of clomiphene citrate treatment. However, a priori …
are responsible for the success or failure of clomiphene citrate treatment. However, a priori …
Contribution of the activities of CYP3A, CYP2D6, CYP1A2 and other potential covariates to the disposition of methadone in patients undergoing methadone …
MR Shiran, MS Lennard, MZ Iqbal… - British journal of …, 2009 - Wiley Online Library
WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT • Several cytochromes P450 (CYPs)
have been implicated in the metabolism of methadone, but there is no consensus on their …
have been implicated in the metabolism of methadone, but there is no consensus on their …
A three-dimensional molecular template for substrates of human cytochrome P450 involved in debrisoquine 4-hydroxylation
SA Islam, CR Wolf, MS Lennard… - …, 1991 - academic.oup.com
A three-dimensional molecular template has been generated for substrates of human
debrisoquine Chydroxylase cytochrome P450 (CYP2D6). This template defines the …
debrisoquine Chydroxylase cytochrome P450 (CYP2D6). This template defines the …
Potent inhibition of yeast-expressed CYP2D6 by dihydroquinidine, quinidine, and its metabolites
…, CL Blake, H Ghabrial, SW Ellis, MS Lennard… - Biochemical …, 1995 - Elsevier
The inhibitory effects of dihydroquinidine, quinidine and several quinidine metabolites on
cytochrome P450 2D6 (CYP2D6) activity were examined. CYP2D6 heterologously expressed …
cytochrome P450 2D6 (CYP2D6) activity were examined. CYP2D6 heterologously expressed …